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Sympathetic Nervous System
- Also known as adrenergic nervous system
- Uses adrenaline (epinephrine) as primary neurotransmitter
- Used in expenditure of energy and response to threatening stimuli
- FIGHT or FLIGHT Reaction
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Parasympathetic Nervous System
- Also known as the cholinergic nervous system
- Uses acetylcholine as primary neurotransmitter
- Used in conservation and restoration of energy
- For rest and digestion
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How does stimulation of the sympathetic nervous system affect each of the following?
- Eye: Dilated pupil (improves far vision)
- Heart: Increased rate of contraction, Increased force of contraction, Coronary artery dilation
- Lungs: Dilation of bronchi
- Blood vessels: Vasodilation, except Kidney
- GI tract: Little effect on muscle tone or secretions, increased sphincter tone
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How does stimulation of the parasympathetic nervous system affect each of the following?
- Eye: Constricted pupil (improves close up vision)
- Heart: Slowed heart rate, Decreased force of contraction, Coronary vasoconstriction
- Lungs: Bronchoconstriction
- blood vessels: No effect, only has effect on skin (Vasodilation)
- GI tract: Increased muscle tone and peristalsis
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Alpha Agonist (Sympathomimetics)
- Ephedrine (Increases blood pressure)
- Clonidine (Centrally acting, decreases blood
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Alpha Antagonist (Blockers, Sympatholytics)
Tamsulosin (Benign prostatic hyperplasia)
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Beta Agonist (Sympathomimetics)
- Beta 2 Selective: lbuterol (Bronchodilator), Salmeterol (Bronchodilator)
- Nonselective: Epinephrine,
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Beta Antagonist (Blockers, Sympatholytics)
- Nonselective: Propranolol
- Beta 1 Selective: Atenolol (Hypertension, angina), Metoprolol (Hypertension, angina)
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Cholinergic Drugs (Parasympathomimetics)
- Direct-Acting; Cholinergic Drugs: Pilocarpine (Glaucoma)
- Indirect-Acting Cholinergic Drugs: Edrophonium (Diagnosis of myasthenia gravis)
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Anticholinergic Drugs (Parasympatholytics):
Tolterodine (Overactive bladder)
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What is heart failure?
- In some patients, the heart looses its ability to pump effectively. This causes the heart to pump out less blood than it receives leading to several undesirable effects:
- left side failure, blood backs up in the lungs and breath difficulties
- right side failure, fluid builds up in the abdominal cavity and legs
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Where does digoxin come from?
- Digitalis purpurea (Foxglove)
- Digitalis lanata (Deadly nightshade)
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How does digoxin work in treating heart failure?
- Increase the force of contraction of the heart
- Decrease heart rate
- Decrease atrioventricular conduction
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What is the usual maintenance dose of digoxin?
- Loading Dose (Digitalization): 0.5 to 1.5 mg in 12-24 hour period.
- Maintenance Dose: 0.125 mg to 0.5 mg/day
- Therapeutic Blood Levels: 1 to 2 mcg/L
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What are some of the signs of digoxin toxicity?
- Nausea and vomiting
- Headache
- Yellow-green visual disturbances, halos
- Cardiac arrhythmia's
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How do potassium levels affect digoxin?
- Low Potassium (Hypokalemia): sensitize the heart to the toxic effects of cardiac glycosides. Increase risk of toxicity Arrhythmia�s and death
- High Potassium (Hyperkalemia): block the therapeutic effects of cardiac glycosides.
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Available agents to treat congestive heart failure
- Digoxin
- Diuretics: Furosemide, hydrochlorothiazide, reduce edema and fluid retention
- ACE Inhibitors: enalapril, lisinopril, ramipril. Decrease blood pressure; allow heart to pump more blood with less effort
- ARB�s: Valsartan and other -sartan
- Carvedilol (Coreg�): nonselective beta blocker and alpha1 receptors, helps the heart work better as a pump
- Nesiritide (Natrecor): recombinant form of human B-type natriuretic peptide (hBNP). Nesiritide relaxes smooth muscle tissue and leads to reduced arterial pressure and improvement in shortness of breath.
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What is angina?
Angina is chest pain caused by insufficient blood flow to the heart muscle.
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What is a myocardial infarction?
Decreased blood flow (ischemia) to the heart results in decreased oxygen available to heart muscle. When oxygen deprivation becomes severe enough, heart muscle may be damaged and myocardial infarction (heart attack) can result.
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What causes angina and/or myocardial infarction?
Decreased blood flow (ischemia) to the heart results in decreased oxygen available to heart muscle. When oxygen deprivation becomes severe enough, heart muscle may be damaged and myocardial infarction (heart attack) can result.
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Why is nitroglycerin useful in angina?
- dilation of arteries and veins.
- decreases the amount of blood returned to the heart
- decreases blood pressure.
- reduce coronary vasospasm
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What are some of the dosage forms available for nitroglycerin?
- Sublingual Nitroglycerin (Nitroquick�): for acute anginal attacks.
- Transdermal Nitroglycerin (Nitro-Dur?, Transderm-Nitro?) to prevent angina attacks.
- Nitroglycerin for IV Infusion: acute events.
- Nitroglycerin Ointment 2%
- Nitroglycerin Extended Release Tablets/Capsules
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Special Storage/Handling Requirements for Nitroglycerin
- Must be stored in light-resistant, airtight containers
- Should not use if tablets are more than 6 months old
- Used transdermal patches still contain small amounts of drugs.
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What other drugs besides nitroglycerin might be used to treat acute coronary syndromes such as angina and myocardial infarction?
- Beta Blockers: prevent or reverse this sympathetic stimulation.
- ACE Inhibitors: lower blood pressure, allowing the heart to pump more blood with less effort.
- ARB�s
- Aspirin: produces a rapid antithrombotic effect.
- Clopidogrel (Plavix�): causes an antithrombotic effect by inhibiting platelet aggregation.
- Ca Channel Blockers: cause vasodilation, decreasing cardiac work and oxygen demand.
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Drugs Used to Treat ACS
- Nitroglycerin(Nitroquick�, Nitro-Dur?, Transderm-Nitro?)
- Isosorbide Dinitrate (Isordil)
- Isosorbide Mononitrate (ISMO�, Imdur?)
- Atenolol (Tenormin�) selective to heart
- Metoprolol (Lopressor?) selective to heart
- Aspirin
- Clopidogrel (Plavix�)
- Amlodipine (Norvasc�)
- Diltiazem (Cardizem?, Dilacor?, Tiazac?)
- Nicardipine (Cardene)
- Nifedipine (Adalat?, Procardia?)
- Verapamil (Calan, Isoptin)
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What are the functions of the kidney?
- Excrete most of the end products of body metabolism
- Control the concentration of most of the constituents of body fluid, a constant blood volume and amounts of solutes in the blood
- Maintain the pressure of blood flow
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Agents Affecting the Proximal Tubule
Acetazolamide (Diamox�): emergency situation, pressure in the eye
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Agents Affecting the Loop of Henle
Furosemide (Lasix�): oral
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Agents Affecting the Distal Tubule
- Hydrochlorothiazide (Hydrodiuril�, Dyazide?, Maxzide)
- Triamterene (Dyazide, Maxzide)
- Metolazone (Zaroxolyn)
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Side effects of Diuretic
- Orthostatic Hypotension: older people tends to have more
- Hyperglycemia
- Potassium Loss
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Spironolactone (Aldactone�)
- Aldosterone Antagonist, Aldosterone causes Na and fluid retention.
- used in conjunction with other diuretics to prevent potassium loss.
- Few side effects, mainly elevated potassium levels.
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Dyazide�, Maxzide�
- Acts directly on the distal convoluted tubules to cause diuresis while inhibiting potassium excretion.
- used in conjunction with other diuretics to prevent potassium loss.
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How do ACE inhibitors work?
- Hypertension
- Congestive Heart Failure
- Post MI
- Increase K level
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How do ARB�s work?
- Angiotensin II Receptor Antagonists
- Hypertension
- Congestive Heart Failure
- Post MI
- Diabetic nephropathy
- Have no effect on k level
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How do direct rennin inhibitors work?
- impacts the rennin/angiotensin system.
- Aliskiren (Tekturna�): Hypertension
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Patients taking which of the following drugs might also need to take a potassium supplement? Furosemide
- Hydrochlorothiazide
- Triamterene, Dyazide�, Maxzide�: Hyperkalemia
- ACE Inhibitors: Hyperkalemia
- ARB�s : has little effect on potassium concentrations.
- Aliskiren (Tekturna�): Hyperkalemia
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What is blood pressure?
Blood pressure is a measurement (usually in millimeters of mercury) of the amount of pressure being exerted on the walls of the arteries by the blood.
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What is high blood pressure? What is hypertension?
Usually defined as blood pressure of greater than 135/90
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Beta-blocker
- Hypertension
- Angina pectoris
- Arrhythmias
- Post myocardial infarction
- Migraine headaches
- Anxiety
- Side effects: Mask the signs of hypoglycemia in patients with diabetes
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Besides B-blockers, what other autonomic nervous system modifiers might be useful in treating hypertension?
- Alpha Blockers: Terazosin (Hytrin?), Doxazosin (Cardura?), Prazosin (Minipres?)
- Alpha Agonists: Clonidine (Catapres?), Guafacine (Tenex?), Guanabenz (Wytensin?)
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Why are calcium channel blockers useful in treating high blood pressure?
When calcium moves through the "slow channels" in the smooth muscles of arteries, vasoconstriction occurs. Calcium channel blockers inhibit this process, thus causing vasodilation.
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Besides high blood pressure, what other things are calcium channel blockers used to treat?
- Arrhythmias
- Angina
- margin headache
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List some of the calcium channel blockers found on our Top 200.
- Amlodipine (Norvasc�)
- Verapamil (Calan, Isoptin)
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What is cholesterol?
Phospholipids
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How is cholesterol useful to the body?
- Help absorb fat
- Necessary for the clotting process
- Part of the sheath that insulates nerve fibers
- Part of the membrane of almost all cells in the body
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How is cholesterol hurtful to the body?
- Atherosclerosis is a condition in which lipid deposits (cholesterol) adhere to the walls of the arteries.
- Atherosclerotic plaques cause the walls of the arteries to become inflexible and thus loose their ability to stretch. Hypertension
- Areas of the arteries where atherosclerotic plaques are present are more likely to rupture. Cerebral hemorrhage, renal hemorrhage, retinal hemorrhage.
- Atherosclerotic plaques can protrude into a vessel and decrease blood flow to the organ or tissue. Angina, ischemia, MI.
- Protruding atherosclerotic plaques make great places for clots to form.
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What are the recommended goals for total cholesterol, LDL cholesterol, HDL cholesterol and triglycerides?
- Total cholesterol: Less than 200 mg/dL
- LDL (bad) cholesterol: Less than 100 mg/dL (70)
- HDL (good) cholesterol: 60 mg/dL or higher (65)
- Triglycerides: Less than 150 mg/dL
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What are some of the factors that can alter lipid levels?
- Increase or decrease in amount of cholesterol ingested: alter LDL cholesterol levels
- Diet high in saturated fat: increase LDL cholesterol levels by about 15 to 25%
- Weight: Losing weight can lower LDL cholesterol and triglycerides while raising HDL cholesterol
- Physical Activity:lower LDL cholesterol and raise HDL cholesterol
- Lack of thyroid: increase LDL cholesterol levels
- Diabetes: LDL cholesterol levels rise very high
- Higher levels of estrogen: decrease LDL cholesterol levels
- Age and Gender: LDL cholesterol levels tend to increase with age
- Heredity
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How do atorvastatin and similar �statin� drugs work?
Inhibit the enzyme HMG Co-A reductase an enzyme required in the formation of cholesterol by the liver. Very effective in lowering LDL cholesterol levels.
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Niacin (Niaspan�):
- Reduces level of plasma proteins that carry cholesterol.
- Lowers LDL cholesterol and triglycerides
- raises HDL cholesterol
- Most common side effects include headache and flushing.
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Bile Sequestering Agents
- Cholestyramine (Questran�)
- Colestipol (Colestid�)
- Bind cholesterol in the GI tract for excretion into the feces.
- Used to lower LDL, cholesterol levels.
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Ezetimibe (Zetia�)
Reduces the absorption of cholesterol from the GI tract.
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Fenofibrate (Tricor�)
- Mainly Inhibits triglyceride synthesis.
- Used to treat elevated triglyceride levels.
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Gemfibrozil (Lopid?)
Used to treat elevated triglyceride levels.
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Heparin
- Inhibits thrombin so that fibrin cannot be formed
- Inhibits thromboplastin so that thrombin cannot be formed
- Interferes with platelet aggregation
- Rapid onset of action (within 5 minutes)
- Short duration of action (2 to 4 hours)
- Cannot be given orally because it is destroyed by gastric acid, IV sub
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warfarin
- The structure of warfarin is very similar to the structure of Vitamin K. When the liver tries to use warfarin instead of Vitamin K to produce clotting factors, abnormal clotting factors are formed.
- Slow onset of action (12 to 72 hours)
- Long duration of action (2 to 10 days), stop it at least one week before op.
- Highly protein bound (this creates lots of drug interactions)
- Very narrow therapeutic range
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Toxicity of Anticoagulant Therapy
- Hemorrhage, bruise, International Normalized Ratio (INR) to reduce.
- Thromboembolism
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What is Trental?? How does it work and what is it used to treat?
- Pentoxifylline (Trental�)
- Reduces blood viscosity
- Improves erythrocyte flexibility
- Indication: intermitted claudication
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What is the dose of Trental?? What dosage forms are available?
- Recommended dose is 400 mg TID, only can change to BID
- Slow onset of action (2 to 4 weeks)
- Controlled release tablet - cannot half
- May cause nausea and vomiting
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How do antiplatelet drugs work? What are they used for?
- Clot formation begins when platelets aggregate or �stick� together. These drugs inhibit platelet aggregation, thus preventing clot formation.
- Prevention of stroke in patients at high risk for stroke or who have previously suffered a stroke (Plavix?, Ticlid?)
- Myocardial infarction prophylaxis (Aspirin - Bayer?, Ecotrin?)
- Intermittent claudication (Pletal?)
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Give an example of an antiplatelet drug on our Top 200?
- Clopidogrel (Plavix?)
- Aspirin (Bayer?, Ecotrin?)
- Cilostazol (Pletal?)
- Prasugrel (Effient)
- Ticlopidine (Ticlid?) amnia,
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What is the immune system?
The human body has the ability to resist almost all types of organisms or toxins that tend to damage the tissues and organs.
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What is an antigen?
- The substances that the immune system attacks.
- Bacteria, Viruses, Toxins
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What is an antibody?
- Humoral Immunity
- B-cells (Bursa of Fabricus)
- Also formed before and shortly after birth
- Fights slowly growing bacteria
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Haptens
- Smaller substances that must combine with a protein to become an antigen.
- Drugs
- Dust
- Dander
- Chemicals
- Smoke
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Where are histamine 1 (H1) receptors found?
- Blood vessels
- Bronchial smooth muscles
- Intestinal smooth muscles
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Where are histamine 2 (H2) receptors found?
- Stomach
- Heart
- Blood vessels
- Uterine tissue
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How do antihistamines work?
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Nonselective antihistamines.
- Promethazine (Phenergan� - used for nausea)
- Tripelennamine (PBZ?)
- Azatadine (Optimine?)
- Azelastine (Astelin? - nasal spray)
- Clemastine (Tavist?)
- Cyproheptadine (Periactin - used for itching, appetite stimulating)
- Dexchlorpheniramine (Polaramine)
- Diphenhydramine (Benadryl) sleep-aid
- Hydroxyzine (Atarax, Vistaril - used for itching, nausea)
- Meclizine (Antivert, used for nausea and dizziness/vertigo)
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selective antihistamines.
- Fexofenadine (Allegra)
- Desloratidine (Clarinex)
- Levocetirizine (Xyzal): OTC
- Bepotastine (Bepreve? - ophthalmic drug)
- Olopatadine (Patanol? - ophthalmic drop, eye contact)
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Why are decongestants often combined with antihistamines? Give an example of a combination antihistamine/decongestant product found on our Top 200 list.
None
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Why are nasal steroids used in patients with allergies? Give an example of a nasal steroid found on our Top 200.
- Intranasal steroids are very effective in preventing acute allergic attacks.
- Budesonide (Rhinocort)
- Fluticasone (Flonase)
- Mometasone (Nasonex)
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Why are antileukotriences used in patients with nasal allergies? Give an example of an antileukotriene found on our Top 200.
- These agents inhibit leukotrienes. Leukotrienes are released in the nasal passages after allergen exposure and lead to the symptoms of allergic rhinitis.
- Montelukast (Singulair)
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Asthma
narrowing of the bronchioles (bronchoconstrictor) due to contraction of smooth muscles. This can be caused by allergies, irritation, exercise, or other factors. It is associated with inflammation.
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Chronic Bronchitis
inflammation of the bronchi. A patient that has excess mucous secretions on most days for 3 months of the year is said to have chronic bronchitis.
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Emphysema
a breakdown in the walls of the alveoli which causes a decrease in oxygen diffusion into the blood. Smoking, miners
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Why are inhaled and oral steroids used in patients with asthma? Give an example of an inhaled steroid found on our Top 200. Give an example of an oral steroid found on our Top 200.
- Steroids decrease bronchoconstriction by decreasing the inflammatory response of the bronchi.
- Oral Steroids: Prednisone (Deltasone�), Methylprednisolone (Medrol�)
- Inhalation Steroids: Fluticasone (Flovent?), Budesonide (Pulmicort?), Triamcinolone (Azmacort?), Flunisolide (Aerobid?), Mometasone (Asmanex?)
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What is theophylline and how is it useful in treating asthma? What side effects might it have?
- Xanthines
- Not sure how these drugs work, they work intracellularly like the beta agonists, thus causing bronchodilation.
- useful for maintenance therapy
- Side effects: Nausea/Vomiting, Increased heart rate, Seizures, Arrhythmia�s
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What other drugs are used to treat asthma? List some that are found on our Top 200.
- Cholinergic Antagonist: Ipratropium (Atrovent�), Tiotropium (Spiriva�)
- Combination Products: Salmeterol/Fluticasone (Advair Diskus�), Albuterol/Ipratropium (Combivent?)
- Antileukotrienes: Montelukast (Singulair?), Zafirlukast (Accolate?), Zileuton (Zyflo?)
- Xanthines: Theophylline (Theo-Dur), Aminophyllin (Aminophylline)
- SRS-A Inhibitor: Cromolyn (Intal)
- Anti-inflammatory: Nedocromil (Tilade)
- Expectorants: Guaifenesin, Iodine
- Mucolytics: Acetylcysteine (Mucomyst?), Dornase Alfa (Pulmozyme?)
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What drugs are used to treat chronic obstructive pulmonary disease? List some that are found on our Top 200?
none
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What is an expectorant?
- Guaifenesin: Decreases viscosity and stickiness of mucus, OTC cough preparations (Robitussin�)
- Iodine: break up mucus. Iodine is secreted in with mucus and breaks it up, making for easier elimination.
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What is a mucolytic?
- used by inhalation. They physically break up mucus for expectoration.
- Acetylcysteine (Mucomyst?): Used for Tylol overdose
- Dornase Alfa (Pulmozyme?)
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